2. Academic Validation
  3. Synthesis and biological evaluation of cis-locked vinylogous combretastatin-A4 analogues: derivatives with a cyclopropyl-vinyl or a cyclopropyl-amide bridge

Synthesis and biological evaluation of cis-locked vinylogous combretastatin-A4 analogues: derivatives with a cyclopropyl-vinyl or a cyclopropyl-amide bridge

  • Bioorg Med Chem Lett. 2009 Mar 1;19(5):1318-22. doi: 10.1016/j.bmcl.2009.01.062.
Nancy Ty 1,  Julia Kaffy,  Alban Arrault,  Sylviane Thoret,  Renée Pontikis,  Joelle Dubois,  Luc Morin-Allory,  Jean-Claude Florent
Affiliations

Affiliation

  • 1 Institut Curie, Centre de Recherche, 26 rue d'Ulm, 75248 Paris, France; CNRS, UMR 176, 26 rue d'Ulm, 75248 Paris, France.
PMID: 19211248 DOI: 10.1016/j.bmcl.2009.01.062
Abstract

A series of novel combretastatin A4 analogues, in which the cis-olefinic bridge is replaced by a cyclopropyl-vinyl or a cyclopropyl-amide moiety, were synthesized and evaluated for inhibition of tubulin polymerization and antiproliferative activity. The derivative 9a with a (cis,E)-cyclopropyl-vinyl unit is the most promising compound. As expected, molecular docking of 9a has shown that only one of the cis-cyclopropyl enantiomers is a good ligand for tubulin.

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